Preparation And Quality Assessment Of Glycyrrhetnic Acid Vesicles Cocoon N-Galactosylated Chitosan Nanoparticles

Objectives and Meaning:In this experiment, lipidvesicles were wrapped on glycyrrhetinic acid N-galactosylated chitosan nanoparticles,to prepare vesicles nanoparticles co-self-assembly architectures with core shell structure. Advantage can be effectively combined with lipid vesicles and nanoparticles to Achieve theeffect ofpassive and actively targeting of combination and the purpose of improve the target of the drug and promote the absorption. To provide an experimental basis for the development that the new dosage forms of traditional Chinese medicine liver targeting.Research method:The glycyrrhetinic acid N-galactosylated chitosan nanoparticles were prepared by ionic cross-linking, orthogonal design optimize the preparation process of the glycyrrhetinic acid N-galactosylated chitosan nanoparticles; The film dispersion-ultrasonic method for the preparation of lipid vesicles, the central composite design-response surface methodology optimize the preparation process of lipid vesicles; The film dispersion-ultrasonic method for the preparation of the glycyrrhetinic acid N- galactosylated chitosan nanoparticles encapsulated in lipid vesicles, The preparation process were optimized through single factor.Appearance ofnanoparticles was observed by transmission electron microscope, The average particle size, Zeta PDI and potential were measured by Zetasizer, Combine Over speed freezing centrifugation and HPLC to the exploration of its encapsulation efficiency and drug loading, Research the drug release behaviorinvitro by reversedialysis method and ultraviolet spectrophotometer method,Comprehensive evaluation of its physical and chemical properties.Research results:Through prescription optimization,the glycyrrhetinic acid N- galactosylated chitosan nanoparticles optimal prescription was as follows: concentration of glycyrrhetinic and N- galactosylated chitosan was 0.2 and 2 mg/m L, ratio of N- galactosylated chitosan and TPP(1.0 mg/m L)_solutions was 20∶3; The glycyrrhetinic acid similar liposome vesicles optimal prescription was as follows: Span-Chol ratio of11:5, hydration temperature was 70℃, hydration time was 51 min, ultrasonic time of 60 min; The similar liposome vesicles cocoon nanoparticles optimal prescription as follows: the vesicles and the quality of the nanoparticles ratioof 8:1, hydration temperature was50℃, hydration time was 40 min. The similar liposome vesicles cocoon nanoparticles,its mean diameter was(414.40±10.98)nm, Zeta potential was-(20.46±0.87)m V, the drug-loading efficiency and encapsulation efficiency were(13.99±0.16)% and(87.19±0.31)%.The release degree of 7.2 within 1 h, The release degree of 76.8within 12 h and 24 h release degree close to 85%.Research conclusion:The glycyrrhetinic acid N-galactosylated chitosan nanoparticles were prepared by ionic cross-linking, preparation of nanoparticle size appropriate, drug loadingand encapsulation efficiency high, prepared process is stable and feasible; The film dispersion-ultrasonic method for the preparation of glycyrrhetinic acid simil-ar liposome vesicles, itsparticle size smaller, encapsulation efficiency higher, and the preparation of similar liposome vesicles cocoon nanoparticle. The particle size was not significantly increase,high encapsulation efficiency and stability of the charge of high potential, and the in vitro release effect is obvious.